METHOD OF PRODUCING [4-(2-CHLORO-4-METHOXY-5- METHYLPHENYL)-5-METHYLTHIAZOLO-2-YL] [2-CYCLOPROPYL-1-(3- FLUORO-4-METHYLPHENYL)-ETHYL]-AMINE Russian patent published in 2014 - IPC C07D277/42 C07D327/04 C07C331/04 

Abstract RU 2523793 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing [4-(2-chloro-4-methoxy-5-methylphenyl)-5-methylthiazolo-2-yl]-[2-cyclopropyl-1-(3-fluoro-4-methylphenyl)-ethyl]-amine of formula (I) (versions) and novel intermediate compounds of the method. The method of producing a compound of formula (I) is carried out by reacting a) a compound of general formula (II), where X denotes halogen, reacting with a thiocyanate of an alkali metal in the presence of a phase-transfer catalyst, and b) reacting the obtained 2-thiocyanate-1-(2-chloro-4-methoxy-5-methylphenyl)-propan-1-one of formula (III) or tautomeric form thereof with 2-cyclopropyl-1-(3-fluoro-4-methylphenyl)-ethylamine of formula (IV). The invention relates to 2-thiocyanate-1-(2-chloro-4-methoxy-5-methylphenyl)-propan-1-one of formula (III) and a tautomer thereof. The invention also relates to a method of producing 2-thiocyanate-1-(2-chloro-4-methoxy-5-methylphenyl)-propan-1-one of formula (III) by reacting a derivative thereof of general formula (II), where X denotes halogen, with a thiocyanate of an alkali metal in the presence of a phase-transfer catalyst.

EFFECT: ecologically clean method of producing the desired compound of formula (I) due to formation of aqueous wastes only, low amount of solvents used to obtain a highly pure product with high output.

13 cl, 7 ex

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RU 2 523 793 C2

Authors

Parkan'I Zhol'T

Fazekas Janosh

Mishkoltsi Peter

Mol'Nar Annamarija

Agai Bela

Dates

2014-07-27Published

2010-04-26Filed